2. Signaling Pathways
  3. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  4. EGFR

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

EGFR

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The EGFR family of receptor tyrosine kinases (RTK) comprises four distinct receptors: the EGFR (also known as ErbB-1/HER1), ErbB-2 (neu, HER2), ErbB-3 (HER3) and ErbB-4 (HER4). All EGFR family members are characterized by a modular structure consisting of an extracellular ligand-binding domain, a single hydrophobic transmembrane region, and the intracellular part harbouring the highly conserved tyrosine kinase domain. The ErbB family of receptor tyrosine kinases (RTKs) couples binding of extracellular growth factor ligands to intracellular signaling pathways regulating diverse biologic responses, including proliferation, differentiation, cell motility, and survival. Ten growth factors and their ErbB specificities are: EGF, amphiregulin (AR), and TGF bind ErbB-1; betacellulin, and epiregulin bind both ErbB-1 and ErbB-4; the neuregulins (also called heregulins and Neu differentiation factors) NRG-1 and NRG-2 bind ErbB-3 and ErbB-4; and NRG-3 and NRG-4 bind ErbB-4. No known ligand binds ErbB-2. The three best characterized signaling pathways induced through ErbBs are Ras-mitogen-activated protein kinase (Ras-MAPK), phosphatidylinositol 3 kinase-protein kinase B (PI3K-PKB/Akt), and phospholipase C-protein kinase C (PLC-PKC) pathways.

EGFR Isoform Specific Products:

EGFR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-E70707
    EGFR L858R Recombinant Human Active Protein Kinase
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L858R Recombinant Human Active Protein Kinase is a recombinant EGFR L858R protein that can be used to study EGFR L858R-related functions.
    EGFR L858R Recombinant Human Active Protein Kinase
  • HY-163419
    HER2-IN-18
    		Inhibitor
    HER2-IN-18 is a HER2 inhibitor, with an IC50 less than 200 nM for HER-YVMA and HER-WT. HER2-IN-18 can be used for cancer research.
    HER2-IN-18
  • HY-162099
    VEGFR-IN-4
    		Inhibitor
    VEGFR-IN-4 (Compound 6e) is an epidermal growth factor receptor (EGFR) inhibitor. VEGFR-IN-4 has potent antiproliferative activity with an IC50 value of 24.6nM against HCC827 cells.
    VEGFR-IN-4
  • HY-146210
    EGFR-IN-50
    		Inhibitor
    EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells.
    EGFR-IN-50
  • HY-142283BS
    N-Desmethyl dosimertinib-d5
    N-Desmethyl dosimertinib-d5 is the deuterium labeled N-Desmethyl dosimertinib.
    N-Desmethyl dosimertinib-d<sub>5</sub>
  • HY-144444
    NSC381467
    		Inhibitor
    NSC381467 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC381467 has strong antiproliferative activities. NSC381467 has the potential for the research of cancer diseases.
    NSC381467
  • HY-146228
    HSP90-IN-13
    		Inhibitor
    HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway.
    HSP90-IN-13
  • HY-RS04473
    Erbb4 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Erbb4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Erbb4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Erbb4 Mouse Pre-designed siRNA Set A
  • HY-138627AR
    AST5902 trimesylate (Standard)
    		Inhibitor
    AST5902 (trimesylate) (Standard) is the analytical standard of AST5902 (trimesylate). This product is intended for research and analytical applications. AST5902 trimesylate is the principal metabolite of Alflutinib (AST2818) both in vitro and in vivo. AST5902 trimesylate exerts antineoplastic activity. Alflutinib is an EGFR inhibitor[1].
    AST5902 trimesylate (Standard)
  • HY-114535
    Jaceidin
    		Inhibitor
    Jaceidin is a promising lead molecule for potent VEGFR inhibitor with excellent membrane permeability and oral bioavailability. Jaceidin exhibits anti-tumor activities.
    Jaceidin
  • HY-P10569
    Biotin HER-2 substrate peptide
    Biotin HER-2 substrate peptide is a substrate of Her4 and Her2/neu tyrosine kinase with a Km value of 60 μm for Her2/neu kinase domain.
    Biotin HER-2 substrate peptide
  • HY-143323
    HER2-IN-9
    		Inhibitor
    HER2-IN-9 is an orally active HER2 inhibitor, with an IC50 value of 0.03 μM. HER2-IN-9 inhibits HER-2 positive breast cancer cells proliferation and migration. HER2-IN-9 can be used in the research of breast cancers.
    HER2-IN-9
  • HY-173367
    Anticancer agent 271
    		Inhibitor
    Anticancer agent 271 (compound 5C) has antiproliferative activity against lung (A549), colon (Caco-2) cancer cell lines, and human lung fibroblast (WI38) with an IC50 value of 9.18 μM on A549 cells. Anticancer agent 271 downregulates PI3K and mTOR gene expression that can be used for cancer research.
    Anticancer agent 271
  • HY-175809
    SRT6
    		Inhibitor
    SRT6, an anticancer agent is a CD44 inhibitor. SRT6 inhibits key CD44-associated kinases, including SRC, ERBB2 and MAPKAPK2. SRT6 has strong tumor selectivity over non-tumoral lung cells and significant antiproliferative activity against cancer cells (EC50of 1.37  μM for NCI-H23 cells).
    SRT6
  • HY-149344
    Anticancer agent 133
    		Inhibitor
    Anticancer agent 133 (compound Rh2) is an anti-cancer agent with cytotoxic and antimetastatic activities. Anticancer agent 133 induces cell cycle arrest, apoptosis, and autophagy. Anticancer agent 133 also inhibits cell metastasis via suppression of EGFR expression mediated by FAK-regulated integrin β1.
    Anticancer agent 133
  • HY-P991236
    MHES0488A
    		Inhibitor
    MHES0488A is a selective humanized antibody that targets HER2 with a KD value of 0.8 nM. MHES0488A is an antibody part of DHES0815A. MHES0488A is internalized by cells and transported to lysosomes, and then releases PBD-monoamide that enters the nucleus, alkylates DNA and induces DNA damage and apoptosis. MHES0488A is promising for research of cancers, such as HER2-positive breast cancer and gastric cancer.
    MHES0488A
  • HY-100064S1
    O-Desmethyl gefitinib-d6
    		Inhibitor
    O-Desmethyl gefitinib-d6 is the deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays.
    O-Desmethyl gefitinib-d<sub>6</sub>
  • HY-172780
    EGFR-IN-161
    		Inhibitor
    EGFR-IN-161 (Compound DD-8) is a potent and reversible inhibitor of L858R/T790M/C797S mutant EGFR kinases, with an IC50 of 0.87 nM. EGFR-IN-161 can induce apoptosis process, G1-phase arrestation, and migration inhibition in tumor cells.
    EGFR-IN-161
  • HY-157166
    EGFR kinase inhibitor 2
    		Inhibitor
    EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S mutants. EGFR kinase inhibitor 2 has the potential to address acquired resistance in the treatment of non-small cell lung cancer.
    EGFR kinase inhibitor 2
  • HY-116277
    Z118332870
    		Inhibitor
    Z118332870 is a potent dual inhibitor of EGFR and BRD4, exhibiting significant potential as a therapeutic agent for overcoming resistance in cancer treatment.
    Z118332870
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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